Scheen A J, Van Gaal L F
Université de Liège, Département de Médecine, Belgique.
Rev Med Liege. 2010 Jul-Aug;65(7-8):464-70.
Liraglutide (Victoza) is a peptide produced by DNA recombinant technology, which presents 97% homology with human glucagon-like peptide-1 (GLP-1) but is resistant to dipeptidylpeptidase-4, the enzyme that degrades the natural hormone. It actives the GLP-1 receptor and exerts an incretin mimetic effect during at least 24 hours after a single subcutaneous injection. Besides a glucose-dependent stimulatory effect of insulin secretion, liraglutide inhibits glucagon secretion and retards gastric emptying. In patients with type 2 diabetes, it reduces glycated haemoglobin by at least 1%, without inducing hypoglycaemia. It also induces a moderate weight loss and a mild reduction in blood pressure. Gastrointestinal adverse events (nausea, vomiting) may occur during the initial phase of treatment, but rarely impose the interruption of the medication and usually diminish with time.Although indicated in combination with other glucose-lowering agents, liraglutide is currently reimbursed in Belgium only if administered in patients with type 2 diabetes not sufficiently controlled with a combination of metformin plus sulfonylurea or metformin plus a thiazolidinedione. Victoza is presented in prefilled pens and is injected subcutaneously once a day. Treatment will be initiated with 0.6 mg to improve digestive tolerance and the daily dose will be increased to 1.2 mg (usual dose) after at least one week, and up to 1.8 mg (maximal dose) if necessary.
利拉鲁肽(维格列汀)是一种通过DNA重组技术生产的肽,与人类胰高血糖素样肽-1(GLP-1)具有97%的同源性,但对二肽基肽酶-4具有抗性,该酶会降解天然激素。它激活GLP-1受体,并在单次皮下注射后至少24小时内发挥肠促胰岛素模拟作用。除了对胰岛素分泌具有葡萄糖依赖性刺激作用外,利拉鲁肽还抑制胰高血糖素分泌并延缓胃排空。在2型糖尿病患者中,它可使糖化血红蛋白降低至少1%,且不会诱发低血糖。它还能导致适度体重减轻和血压轻度降低。胃肠道不良事件(恶心、呕吐)可能在治疗初期出现,但很少导致停药,通常会随着时间推移而减轻。虽然利拉鲁肽可与其他降糖药物联合使用,但目前在比利时,仅当用于使用二甲双胍加磺脲类药物或二甲双胍加噻唑烷二酮类药物联合治疗仍控制不佳的2型糖尿病患者时,该药才可报销。维格列汀预装在笔式注射器中,每天皮下注射一次。治疗起始剂量为0.6毫克,以提高消化耐受性,至少一周后每日剂量将增加至1.2毫克(常用剂量),必要时可增至1.8毫克(最大剂量)。